JP5624148B2 - 大環状インテグラーゼ阻害剤 - Google Patents

大環状インテグラーゼ阻害剤 Download PDF

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JP5624148B2
JP5624148B2 JP2012533614A JP2012533614A JP5624148B2 JP 5624148 B2 JP5624148 B2 JP 5624148B2 JP 2012533614 A JP2012533614 A JP 2012533614A JP 2012533614 A JP2012533614 A JP 2012533614A JP 5624148 B2 JP5624148 B2 JP 5624148B2
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mmol
compound
naphthyridine
methyl
mixture
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JP2013507423A5 (es
JP2013507423A (ja
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ヨハネス・ウィルヘルムス・イェー・チューリング
ジャン−フランソワ・ボンファンティ
ジェローム・ミシェル・クロード・フォルタン
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エランコ・アニマル・ヘルス・アイルランド・リミテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D513/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4375—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a six-membered ring having nitrogen as a ring heteroatom, e.g. quinolizines, naphthyridines, berberine, vincamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains three hetero rings
    • C07D471/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains four or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D515/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D515/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen, oxygen, and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains three hetero rings
    • C07D515/18—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
JP2012533614A 2009-10-13 2010-10-13 大環状インテグラーゼ阻害剤 Active JP5624148B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09172853.5 2009-10-13
EP09172853 2009-10-13
PCT/EP2010/065300 WO2011045330A1 (en) 2009-10-13 2010-10-13 Macrocyclic integrase inhibitors

Publications (3)

Publication Number Publication Date
JP2013507423A JP2013507423A (ja) 2013-03-04
JP2013507423A5 JP2013507423A5 (es) 2013-11-21
JP5624148B2 true JP5624148B2 (ja) 2014-11-12

Family

ID=41720665

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JP2012533614A Active JP5624148B2 (ja) 2009-10-13 2010-10-13 大環状インテグラーゼ阻害剤

Country Status (15)

Country Link
US (1) US8497270B2 (es)
EP (1) EP2488521B1 (es)
JP (1) JP5624148B2 (es)
KR (1) KR20120087916A (es)
CN (1) CN102574854B (es)
AU (1) AU2010305805B2 (es)
BR (1) BR112012008586A2 (es)
CA (1) CA2777664C (es)
EA (1) EA019558B1 (es)
ES (1) ES2446720T3 (es)
IL (1) IL218845A0 (es)
MX (1) MX2012004426A (es)
NZ (1) NZ598766A (es)
WO (1) WO2011045330A1 (es)
ZA (1) ZA201202516B (es)

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WO2014008636A1 (en) * 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
US9714243B2 (en) 2012-12-17 2017-07-25 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as HIV integrase inhibitors
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
HUE036384T2 (hu) 2013-05-17 2018-07-30 Merck Sharp & Dohme Fúzionált triciklusos heterociklikus vegyületek mint HIV integráz inhibitorok
EP3008044B1 (en) 2013-06-13 2018-11-21 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
MD4794B1 (ro) 2013-09-27 2022-02-28 Merck Sharp & Dohme Corp Derivaţi de chinolizină substituiţi utili ca inhibitori de integrază HIV
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
WO2017004342A1 (en) 2015-07-02 2017-01-05 Tp Therapeutics, Inc. Chiral diaryl macrocycles as modulators of protein kinases
DK3325488T3 (da) 2015-07-21 2020-09-14 Turning Point Therapeutics Inc Chiral diaryl-makrocyklus og anvendelse deraf til behandling af cancer
EP3377066B1 (en) 2015-11-17 2021-04-07 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as hiv integrase inhibitors
WO2017106071A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Spirocyclic quinolizine derivatives useful as hiv integrase inhibitors
WO2017113288A1 (en) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
BR112019011074B1 (pt) 2016-12-02 2021-01-19 Merck Sharp & Dohme Corp. Compostos heterocíclicos tricíclicos inibidores de hiv integrase, composição que oscompreende e uso dos mesmos
TWI808958B (zh) 2017-01-25 2023-07-21 美商特普醫葯公司 涉及二芳基巨環化合物之組合療法
EP3573984A4 (en) 2017-01-26 2020-07-29 Merck Sharp & Dohme Corp. USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
IL271964B1 (en) 2017-07-28 2024-08-01 Turning Point Therapeutics Inc Macrocyclic compounds and their uses
SI3728271T1 (sl) 2017-12-19 2023-01-31 Turning Point Therapeutics, Inc. Makrociklične spojine za zdravljenje bolezni
TWI745900B (zh) 2019-03-22 2021-11-11 美商基利科學股份有限公司 橋鍵聯三環胺甲醯吡啶酮化合物及其醫藥用途
PE20221569A1 (es) 2020-02-24 2022-10-06 Gilead Sciences Inc Compuestos tetraciclicos para el tratamiento de infecciones por vih
KR20230079137A (ko) * 2020-09-30 2023-06-05 길리애드 사이언시즈, 인코포레이티드 가교된 트리사이클릭 카르바모일피리돈 화합물 및 이의 용도
CN112358477A (zh) * 2020-11-10 2021-02-12 牡丹江医学院 一种用于治疗胆囊炎的药物及其制备方法
ES2968058T3 (es) 2021-01-19 2024-05-07 Gilead Sciences Inc Compuestos de piridotriazina sustituidos y usos de los mismos
TWI843506B (zh) 2022-04-06 2024-05-21 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途
CN115974886A (zh) * 2022-11-22 2023-04-18 国科大杭州高等研究院 一种含有二氢苯并呋喃骨架的大环内酰胺化合物及其制备方法

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Publication number Publication date
AU2010305805A1 (en) 2012-04-19
CN102574854B (zh) 2014-04-16
ES2446720T3 (es) 2014-03-10
KR20120087916A (ko) 2012-08-07
IL218845A0 (en) 2012-06-28
US8497270B2 (en) 2013-07-30
EP2488521B1 (en) 2013-12-18
CA2777664A1 (en) 2011-04-21
BR112012008586A2 (pt) 2016-11-29
WO2011045330A1 (en) 2011-04-21
MX2012004426A (es) 2012-07-30
CN102574854A (zh) 2012-07-11
JP2013507423A (ja) 2013-03-04
EP2488521A1 (en) 2012-08-22
EA019558B1 (ru) 2014-04-30
EA201270540A1 (ru) 2012-09-28
AU2010305805B2 (en) 2014-04-03
ZA201202516B (en) 2013-09-25
CA2777664C (en) 2014-06-10
US20120172367A1 (en) 2012-07-05
NZ598766A (en) 2013-09-27

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